Composition for intestinal delivery

Abstract

The present invention relates to a new composition, use and method for oral administration to a human or an animal of a physiologically active agent comprising neutralizing agents to increase pH in the digestive system to prevent denaturation, inhibitors of digestive enzymes to substantially prevent enzymatic digestion, and at least uptake increasing agents which increases intestinal absorption of a physiologically active agent, a drug and/or a nutrient.

Description

RELATED APPLICATIONS [0001] This application is a continuation of pending application Ser. No. 10 / 181,428, filed Jan. 25, 2001, entitled “COMPOSITION FOR INTESTINAL DELIVERY” which is a US national phase of PCT / CA01 / 00073 filed Jan. 25, 2001, which claimed priority to U.S. Provisional application No. 60 / 178,318 filed Jan. 27, 2000, which are hereby incorporated by reference into this application.BACKGROUND OF THE INVENTION [0002] (a) Field of the Invention [0003] The present invention relates to a composition and a method for oral administration of physiological active products and intestinal delivery thereof. The physiological active products administered with the present invention allows to achieve a better systemic delivery and, immunologic induction, and has demonstrated improved nutritional, nutraceutical, and therapeutic capacities. [0004] (b) Description of Prior Art [0005] The conventional route of therapy involving protein or peptide drugs is via parenteral administration (...

AI Technical Summary

Benefits of technology

[0058] The term “therapeutically effect amount” of a medicament is meant a sufficient amount of the compound to obtain the intended therapeutic benefit, at a reasonable benefit/risk ratio applicable to any medical treatment. It will be understood, however, that the total daily usage of the medicaments and compositions of the present invention will be decided by the attending physician with the scope of sound medical judgement. The specific therapeutically effective dose level for any particular patient will depend upon a variety of factors including the disorder being treated and the severity of the disorde

Problems solved by technology

This is primarily due to the lack of absorption of such drugs through the gastrointestinal tract.

However, injections are painful and sometimes difficult to administer relative to other dosage forms.

However, delivery of therapeutic polypeptides through the gastrointestinal (GI) tract has a number of problems such as low pH in the stomach, proteolytic degradation of the drug in the small intestine, low absorption through the intestinal membrane, and limited stability of such formulations, especially as an aqueous solution, which are all potential barriers to absorption of polypeptides following oral administration.

This is a particular problem with proteins and polypeptides which, even with the advent of biotechnology, are still of relatively limited availability and are complex chemical entities as well, and very expensive as a result.

Additionally, the liquid or semi-solid compositions of the prior art are difficult to formulate or package into a dosage form for oral delivery.

The combination of a low pH and peptic activity probably results in denaturation of most food proteins, exposing bonds susceptible to further hydrolysis within the small intestine.

Hence, these mechanisms inevitably pose considerable difficulty for the invention of effective modes of delivery for peptide and protein drugs.

On the other hand, entry of some intact peptides and proteins to the circulation may be detrimental, although factual proof of this is currently incomplete, and many claims of

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